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Bioabsorbable Polymer
Poly(DL-Lactide-co-Glycolide)
APPLICATIONS (Examples 1)
Anti-Cancer Drug
US 5304377
US 5603961
APPLICATIONS (Examples 2)
GnRH analogues for prostate cancer
ZOLADEX(AstraZeneca) Pellet of Goserelin acetate with PLGA
Control of releasing time of the drug (interval 28days 12weeks Prolong the anti-cancer effect
Microsphere
Formulation (1)
Emulsion O/W
Polymer, Drug, Organic solvent
O = Oil W = Water
Solvent
elimination
Filtration Drying
Microsphere
Water
O/W Emulsion
W/O/W
Drug, Water
Microsphere
Formulation (2)
Fusion
Polymer Heating Fusion Drug Mixing
Strand
Ground, Drying
Microsphere
Spray dry
Polymer Heating Fusion Drug Mixing
MITSUI CHEMICALS, INC. HEALTH CARE MATERIALS DIVISION
Spray Drying
Microsphere
80 60 40 20 0 0 20
Days
40
60
PLGA 5-50 PLGA 75-65
MITSUI CHEMICALS, INC. HEALTH CARE MATERIALS DIVISION
Mw Retention (%)
80 60
40
20
40 20
0 0 20
Days
40
60
PLGA 5-50 PLGA 75-65
MITSUI CHEMICALS, INC. HEALTH CARE MATERIALS DIVISION
Physical Properties
PGA
CAS No. Chemical Formula Color Odor TmMelting PointC TgGlass Transition C Solubility 26202-08-4
PLGA 5
26780-50-7
PLGA 75
( C4H4O4 )x
light tan
( C4H4O4 )x ( C6H8O4 )y
white to light tan
Odorless 220-230
Odorless
35-40
HFIP
45-55
CH2Cl2 CHCl3 DMF DMSO THF
Properties
Polymer Co-polymer ratiomol% *Inherent Viscosity **Molecular Weight Residual monomer % Sn content Heavy metals Sulphated ash
GLD
PGA 100
LTD( form)
dL/g
0.90 1.10
kDa
(100)
GLD
< 1.0
LTD
ppm
< 10
ppm
< 10
%
< 0.1
PLGA 5-50
PLGA 75-75 PLGA 75-65 PLGA 75-50
45 55
45 55(DL)
0.45 0.60
0.72 0.80
(50 55)
(78 85) (62 76) (50 60)
< 2.0
< 2.0
< 50
< 10
< 0.1
20 30
70 80(DL)
< 2.0
< 2.0
< 50
< 10
< 0.1
*Inherent viscosity
GRADE
Standard grade PLGA 5-50 is a product with the decomposition rate of one month, and PLGA 75-65 is a product decomposing in three months. PLGA 75-50, PLGA 75-65 and PLGA75-75 which decompose slower than PLGA 5-50. Upon request, the products of which physical properties and inherent viscosity are partially altered, are available as a special grade. One of the characteristics of our PLGA is that no solvent remaining in this product. This is due to our unique manufacturing method which does not contain solvent in the manufacturing and purifying processes.
GMP & DMF The PLGA series are manufactured at our cGMP plant in Nagoya Works Drug Master File is filed to FDA and Medicine Control Agency of U.K., Product Master File is filed to Canadian Authority in 5 and 75 type respectively
H C H Hydrolysis
O C OH
PGA
[CAS No. 26202-08-4]
Glycolic Acid
PLGA
[CAS No. 2678050-7]
H HO C CH3
O C OH
Lactic Acid
GLD GLD
O H3C O O O CH3
Catalyst Initiator
Polymerization
Removal of Monomers
Pelletization or Crashing
LTD
CHCOCHCO
CH3 CH3 l
CHCOCHCO H H m n
MITSUI CHEMICALS, INC. HEALTH CARE MATERIALS DIVISION
PLGA